新型咪唑啉酮类Schiff碱的合成及其生物活性

新型咪唑啉酮类Schiff碱的合成及其生物活性;串联aza-Witing反应     

2-烷氧基-4H-咪唑啉-4-酮衍生物的合成与杀菌活性

应用烯基膦亚胺（1）与芳基异氰酸酯的氮杂Wittig反应，得到的碳二亚胺2再 与醇在醇钠催化下反应，合成了新的2-烷氧基-4H-咪唑啉-4-酮衍生物（3），探讨 了成环反应的条件以及所合成的新型杂环化合物的杀菌活性，结果表明部分化合物 表现出较好的抑菌活性，其中以3b活性最好，在50 mg/L浓度时，对水稻纹枯菌和 苹果轮纹菌的抑制率达81%以上。     

New Facile Synthesis of 2-Aryloxy-5-(2-furfurylidene)- 4H-imidazolin-4-ones

Many N-heterocycles including 4H-imidazolin-4-ones exhibit biological activities1-3. Some derivatives of 5-(2-furfurylidene)-4H-imidazolin-4-one were found to show good antiinflammatory activity4. They can be synthesized by condensation of furfural with 5- unsubsituted 4H-imidazolin-4-ones or from corresponding oxazolones5,6. However, no synthesis of 2-aryloxy substituted 5-(2-furfurylidene)-4H-imidazolin-4-one was reported. Recently, aza-Wittig reaction has received increased attention …     

2-烷氧基-3H-喹唑啉-4-酮的合成与杀菌活性

研究了合成2-烷氧基-3H-喹唑啉-4-酮衍生物4的方法,该方法应用膦亚胺1与芳基异氰酸酯的氮杂Wittig反应,得到的碳二亚胺2再与醇在醇钠催化下反应,合成了12种未见文献报道的喹唑啉酮衍生物4.所得产物4的结构由NMR,MS,IR所确证.探讨了成环反应的条件以及所合成的新型杂环化合物的杀菌活性,结果表明部分化合物表现出较好的抑菌活性,如41在50 mg/L浓度时,对水稻纹枯菌的抑制率为89%.     

SYNTHESIS AND FUNGICIDAL ACTIVITIES OF 2-BENZOTHIAZOLYLTHIO-SUBSTITUTED 4H-IMIDAZOL-4-ONES AND 4(3H)-QUINAZOLINONES

4H-Imidazol-4-ones 4 or 4(3H)-quinazolinones 8 were synthesized by base catalytic reactions of 2-mercaptobenzothiazole with carbodiimides 2 or 6, respectively, which were obtained via aza-Wittig reaction of iminophosphorane 1 or 5 with aromatic isocyanates. 4 and 8 exhibited fungicidal activity.     

(N-Isocyanimino)triphenylphosphorane-Mediated,One-Pot,Efficient Synthesis of Sterically Congested 1,1,1-Trifluoro-2-(5-aryl-1,3,4-oxadiazol-2-yl)-2-propanol Derivatives via Intramolecular Aza-Wittig Reaction

Reactions of (N-isocyanimino)triphenylphosphorane with 1,1,1-trifluoroacetone in the presence of aromatic (or heteroaromatic) carboxylic acids (3-methylbenzoic acid, 1-naphthalenecarboxylic acid, 2-naphthalenecarboxylic acid, 2-furancarboxylic acid, and 2-thiophenecarboxylic acid) proceed smoothly at room temperature and in neutral conditions to afford sterically congested 1,1,1-trifluoro-2-(5-aryl-1,3,4-oxadiazol-2-yl)-2-propanol derivatives in high yields. The reaction proceeds smoothly and cleanly under mild conditions, and no side reactions were observed.

Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.     

One-Pot Synthesis and Fungicidal Activities of Derivatives of Imidazo [2,1-b]-1,3,4-thiadiazol-5(6H)-one

The isothiocyanates 2, obtained from aza-Wittig reactions of vinyliminophosphoranes 1 with CS ₂ , reacted with hydrazine to give 3-amino-2-thioxo-4-imidazolidinones 4. One-pot reactions of 4, aromatic isocyanates, Ph ₃ P, C ₂ Cl ₆ , and Et ₃ N generated imidazo[2,1-b]-1,3,4-thiadiazol-5(6H)-ones 7. Compound 7 exhibited good fungicidal activities, especially against Sclerotinia sclerotiorum de Bary and Botrytis Cinerea Pers.     

2-胺基(芳氧基)-5,8,9-三甲基噻吩并吡啶并[4,3-d]嘧啶-4(3H)-酮的合成和生物活性

利用串联Aza-Wittig法合成了两类共计16个未见文献报道的噻吩并吡啶并嘧啶类化合物, 通过IR, ¹H NMR, EI-MS, 元素分析等方法对所合成的化合物进行了结构表征, 化合物II-1还通过了X单晶衍射的进一步确证. 并初步测定了所合成化合物的杀虫、杀菌和除草活性. 结果表明: 所测化合物的杀虫活性较差, 但大部分化合物具有一定的除草活性和良好的杀菌活性.     

N-isocyaniminotriphenylphosphorane (Ph3PNNC) as an efficient reagent for the synthesis of ferrocene-containing 1,3,4-oxadiazole derivatives

Reaction of N-isocyaniminotriphenylphosphorane (Ph₃PNNC) with an aromatic aldehyde in the presence of ferrocene carboxylic acid and a secondary amine proceeds smoothly at room temperature under neutral conditions to afford sterically congested ferrocene-containing 1,3,4-oxadiazole derivatives in high yields. The reaction progresses smoothly and clearly under mild conditions and no side reactions were observed.     

噻吩并嘧啶酮衍生物的合成及其抑菌活性

利用三组分氮杂Wittig反应,以磷亚胺2、对氯苯基异氰酸酯和酚,合成了16个未见文献报道的2-芳氧基-3-对氯苯基-3,5,6,7-四氢-4H-环戊二烯并[4,5]噻吩并[2,3-d]-嘧啶-4-酮衍生物,产率52～74%。通过IR、1H NMR、MS和元素分析对目标化合物的结构进行了表征。初步探讨了所合成化合物的抑菌活性,结果显示所合成的化合物对真菌的抑制活性优于对细菌的抑制活性,对桔青霉菌的抑制活性在65.2%以上,其中5n的抑菌率最高,达到89.1%。在化合物对细菌的抑制活性中,对绿脓杆菌的抑菌率较好,在52.8～73.0%之间,对金黄色葡萄球菌的抑制活性最低,在43.3～65.5%之间。